Merck + Co., Inc.

David C Remy

John J Baldwin

David A Claremon

Harold G Selnick

Jason M Elliott

Gerald S Ponticello

Nigel J Liverton

Stella W King

Paul S Anderson

Ben E Evans

Joseph G Atkinson

Marcia E Christy

Paul A Friedman

Clarence S Rooney

Patrice C Belanger

Edward L Engelhardt

Andrew M Stern

Bradley V Clineschmidt

Mark G Bock

Roger M Freidinger

Samuel L Graham

Steven D Young

Susan F Britcher

Robert M DiPardo

Stanley F Barnett

Gabriel F Eilon

Mark B Freedman

Mark Johnson

The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention

Inhibitors of Akt activity

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Nitrogen-containing spirocycles

Benzodiazepines

Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.

Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

Antiarrhythmic benzodiazepines

This invention is concerned with novel compounds represented by structural formulae I and II. ##STR1## which are useful in the treatment of cardiac arrhythmia.

Furanodiazepines

Imidazobenzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

Benzodiazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

3-Acylamino-5-Aminobenzo[1,5]diazepines are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

3-acylaminobenzodiazepines

Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.

Adjuncts in cancer chemotherapy

Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R.sup.2 and R.sup.3 are H, substituted or unsubtituted C.sub.1-3 alkyl, C.sub.1-3 alkoxy, N(R).sub.2, halogen, CF.sub.3 or R.sup.5 and R.sup.1 is H or an aryl group.

Nitrogen-containing heterocyclic compounds as class III antiarrhythmic

Certain Factor XIIIa inhibitor compounds have been discovered which have been found to be useful in the lysis of blood clots and thus adaptable for administration in thrombolytic therapy either alone or together with plasminogen activator.

Growing community of inventors

North Wales, PA, United States of America

David C Remy